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1. 发明申请

WO2006115834A1 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2006115834A1
公开(公告)日：2006-11-02
申请号：PCT/US2006/014092
申请日：2006-04-14
申请人： MERCK & CO., INC. , ALANI, Laman, L. , DUBOST, David, C. , FOSTER, Bruce, S. , GHOSH, Soumojeet , JAHANSOUZ, Hossain , POURKAVOOS, Nazaneen , REGE, Bhagwant , TATAVARTI, Aditya
发明人： ALANI, Laman, L. , DUBOST, David, C. , FOSTER, Bruce, S. , GHOSH, Soumojeet , JAHANSOUZ, Hossain , POURKAVOOS, Nazaneen , REGE, Bhagwant , TATAVARTI, Aditya
IPC分类号： A61K31/41 , C07D257/04
CPC分类号： C07D403/10
摘要： The compounds of the present invention are polymorphic crystalline forms of the compound 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid, which has the structure (I). Specifically, the compounds of the invention are selected from the group consisting of 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid of Claim 3 selected from the group consisting of 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form I, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form II, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form III, and 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form IV, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form V, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VI, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VII, and 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VIII.
摘要翻译：本发明的化合物是2-丁基-4-氯-1 - （（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-1-基的化合物的多晶型形式，其具有结构（I）。具体地说，本发明化合物选自2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑 -5-羧酸，其选自2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑 -5-甲酸盐酸盐形式I，2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸盐酸盐形式II，2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸盐酸盐形式III和 2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式IV，2-丁基-4 - 氯 - 1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式V，2-丁基-4-氯-1- 甲基] - 咪唑-5-羧酸一水合物形式VI，2-丁基-4-氯-1 - [（2' - （1H-四唑-5-基）联苯-4-基）（1-1H-四唑-5-基）联苯-4-基）甲基]咪唑-5--C 羧酸一水合物形式VII和2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式八。

2. 发明申请

WO2009117278A2 PROCESSES FOR PREPARING (AMINO-PYRAZOLOPYRIDINYL)METHOXY SUBSTITUTED BIARYL ETHERS 审中-公开
标题翻译：制备（氨基 - 吡唑并吡啶-2-基）甲氧基取代二异氰酸酯的方法
公开(公告)号：WO2009117278A2
公开(公告)日：2009-09-24
申请号：PCT/US2009/036616
申请日：2009-03-10
申请人： MERCK & CO., INC. , KUETHE, Jeffrey, T. , ZHONG, Yong Li , YASUDA, Nobuyoshi , TUCKER, Thomas, J. , PYE, Philip , ZHANG, Yangfeng , TYNEBOR, Robert , DUBOST, David, C. , BEUTNER, Gregory, L. , TELLERS, David, M.
发明人： KUETHE, Jeffrey, T. , ZHONG, Yong Li , YASUDA, Nobuyoshi , TUCKER, Thomas, J. , PYE, Philip , ZHANG, Yangfeng , TYNEBOR, Robert , DUBOST, David, C. , BEUTNER, Gregory, L. , TELLERS, David, M.
IPC分类号： A61P31/18 , C07D213/61 , C07D213/74 , C07D471/04
CPC分类号： C07D213/61 , C07D213/74 , C07D471/04 , Y02P20/55
摘要： Processes for preparing certain (amino-pyrazolopyridinyl)methoxy-substituted biaryl ethers and their salts are described. The substituted biaryl ethers are useful as HIV non-nucleoside reverse transcriptase inhibitors. The processes include coupling a biaryl ether with a suitably protected and activated pyrazolopyridinyl methanol and then removing the protective groups from the coupled product to provide the desired substituted biaryl ether in the form of a sulfonate salt or a sulfate salt. Earlier reaction steps and the intermediates employed and obtained therein are also described. Crystalline HCl and sulfate salts of a particular (amino-pyrazolopyridmyl)-methoxy~substituted biaryl ether are described as well.
摘要翻译：描述了制备某些（氨基 - 吡唑并吡啶基）甲氧基取代的联芳基醚及其盐的方法。取代的联芳基醚可用作HIV非核苷逆转录酶抑制剂。这些方法包括将联芳基醚与适当保护的和活化的吡唑并吡啶基甲醇偶联，然后从偶联产物中除去保护基团，以提供磺酸盐或硫酸盐形式的所需取代的联芳基醚。还描述了早期反应步骤及其中使用和获得的中间体。还描述了特定（氨基 - 吡唑并吡啶基） - 甲氧基 - 取代的联芳基醚的结晶HCl和硫酸盐。

3. 发明申请

WO2010042392A2 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：艾滋病毒整合抑制剂
公开(公告)号：WO2010042392A2
公开(公告)日：2010-04-15
申请号：PCT/US2009/059308
申请日：2009-10-02
申请人： MERCK & CO., INC. , ISAACS, Richard, C. A. , THOMPSON, Wayne, J. , WILLIAMS, Peter, D. , SU, Dai-Shi , VENKATRAMAN, Shankar , EMBREY, Mark, W. , FISHER, Thorsten, E. , WAI, John, S. , DUBOST, David, C. , BALL, Richard, G. , CHOI, Eric, J. , PEI, Tao , TRICE, Sarah, L. , CAMPBELL, Neil , MADDESS, Matthew , MALIGRES, Peter, E. , SHEVLIN, Michael , SONG, Zhiguo Jake , STEINHUEBEL, Dietrich, P. , STROTMAN, Neil, A. , YIN, Jingjun
发明人： ISAACS, Richard, C. A. , THOMPSON, Wayne, J. , WILLIAMS, Peter, D. , SU, Dai-Shi , VENKATRAMAN, Shankar , EMBREY, Mark, W. , FISHER, Thorsten, E. , WAI, John, S. , DUBOST, David, C. , BALL, Richard, G. , CHOI, Eric, J. , PEI, Tao , TRICE, Sarah, L. , CAMPBELL, Neil , MADDESS, Matthew , MALIGRES, Peter, E. , SHEVLIN, Michael , SONG, Zhiguo Jake , STEINHUEBEL, Dietrich, P. , STROTMAN, Neil, A. , YIN, Jingjun
IPC分类号： A61K31/553 , C07D487/04 , C07D281/10 , A61K31/55 , A61P31/18
CPC分类号： C07D498/04 , C07D487/04 , H01L2924/0002 , H01L2924/00
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I), wherein X 1 , X 2 , Y, R 1A , R 1B , R 2 and R 3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.
摘要翻译：式I化合物是HIV整合酶抑制剂和HIV复制抑制剂：（I），其中X1，X2，Y，R1A，R1B，R2和R3如本文所定义。该化合物可用于预防或治疗艾滋病毒感染，并预防，治疗或延迟艾滋病的发病或进展。该化合物用作抗体作为化合物本身（或其水合物或溶剂化物）或以药学上可接受的盐形式的HIV感染和AIDS。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。还描述了制备式I化合物的方法及其中间体。

4. 发明申请

WO2008013807A9 A NOVEL LACTIC ACID FORMULATION OF MK-0457 USEFUL FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2008013807A9
公开(公告)日：2008-01-31
申请号：PCT/US2007/016637
申请日：2007-07-24
申请人： MERCK & CO., INC. , DUBOST, David, C.
发明人： DUBOST, David, C.
IPC分类号： A61K47/12 , A61K31/506 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/14 , A61K9/16 , A61K9/00 , A61P35/00 , A61P35/02
摘要： A lactic acid formulation, and a process to prepare that formulation, of MK-0457 is disclosed:. Such a formulation is useful in the treatment of cancer.

5. 发明公开

EP1874302A1 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译：血管紧张素II受体拮抗剂
公开(公告)号：EP1874302A1
公开(公告)日：2008-01-09
申请号：EP06750200.5
申请日：2006-04-14
申请人： Merck & Co., Inc.
发明人： ALANI, Laman, L. , DUBOST, David, C. , FOSTER, Bruce, S. , GHOSH, Soumojeet , JAHANSOUZ, Hossain , POURKAVOOS, Nazaneen , REGE, Bhagwant , TATAVARTI, Aditya
IPC分类号： A61K31/41 , C07D257/04
CPC分类号： C07D403/10
摘要： The compounds of the present invention are polymorphic crystalline forms of the compound 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid, which has the structure (I). Specifically, the compounds of the invention are selected from the group consisting of 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid of Claim 3 selected from the group consisting of 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form I, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form II, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form III, and 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form IV, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form V, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VI, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VII, and 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VIII.

6. 发明公开

EP1019402A1 POLYMORPHIC FORMS OF A GROWTH HORMONE SECRETAGOGUE 失效
标题翻译：多晶型生长激素BEFÖRDERENDCONNECTION
公开(公告)号：EP1019402A1
公开(公告)日：2000-07-19
申请号：EP96936869.5
申请日：1996-10-23
申请人： MERCK & CO., INC.
发明人： DRAPER, Jerome, P. , DUBOST, David, C. , KAUFMAN, Michael, J. , MCCAULEY, James, A. , VANDRILLA, Jennifer, L. , VARSOLONA, Richard, J.
IPC分类号： C07D471/10 , A61K31/445
CPC分类号： C07D471/10 , A61K38/00 , C07K5/06034
摘要： This invention is concerned with polymorphic forms of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonylspiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyloxy)ethyl]-2-amino-2-methylpropanamide methanesulfonate which is a growth hormone secretagogue that is useful in food animals to promote their growth thereby rendering the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, and to treat medical conditions which are improved by the anabolic effects of growth hormone. The instant polymorphic forms have advantages over the other known forms of N-[1(R)-[(1,2-dihydro-1-methanesulfonylspiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyloxy)-ethyl]-2-amino-2-methylpropanamide methanesulfonate in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations. The present invention is also concerned with processes for preparing these polymorphic forms, pharmaceutical formulations comprising these polymorphic forms as active ingredients and the use of the polymorphic form of the compound and their formulations in the treatment of certain disorders.

7. 发明公开

EP2051737A2 A NOVEL LACTIC ACID FORMULATION OF MK-0457 USEFUL FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的MK-0457的新配方乳酸
公开(公告)号：EP2051737A2
公开(公告)日：2009-04-29
申请号：EP07796994.7
申请日：2007-07-24
申请人： Merck & Co., Inc.
发明人： DUBOST, David, C.
IPC分类号： A61K47/12 , A61K31/506 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/14 , A61K9/16 , A61K9/00
CPC分类号： A61K9/0019 , A61K9/10 , A61K9/107 , A61K9/1075 , A61K9/485 , A61K9/4858 , A61K31/506 , A61K47/12
摘要： A lactic acid formulation, and a process to prepare that formulation, of MK-0457 is disclosed:. Such a formulation is useful in the treatment of cancer.

8. 发明公开

EP0857020A1 WET GRANULATION FORMULATION OF A GROWTH HORMONE SECRETAGOGUE 失效
标题翻译：一种生长激素分泌物的湿式制粒方法
公开(公告)号：EP0857020A1
公开(公告)日：1998-08-12
申请号：EP96937761.0
申请日：1996-10-23
申请人： MERCK & CO., INC.
发明人： ASGHARNEJAD, Mandana , DRAPER, Jerome, P. , DUBOST, David, C. , KAUFMAN, Michael, J. , STOREY, David, E.
IPC分类号： C07D471 , A61K9 , A61K31 , A61K47
CPC分类号： A61K31/438 , A61K9/2004 , A61K9/2077
摘要： The present invention relates to a pharmaceutical composition and a process for the preparation of a tablet containing a growth hormone secretagogue as the active ingredient. The tablet is prepared by forming a powder blend of the active ingredient N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methyl-propanamide, or a pharmaceutically acceptable salt thereof, in particular the methanesulfonate salt, with a binder/diluent, a first diluent, a second diluent, a first portion of a disintegrant, and a lubricant; wet granulating the powder blend with a solution of ethanol/water to form granules; drying the granules to remove the ethanol/water; adding a second portion of a disintegrant; lubricating the granules; and compressing the dried granules into the desired tablet form. The present invention further relates to a novel amorphous form of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methylpropanamide methanesulfonate which is produced directly as a result of the process of tablet formulation.
摘要翻译：本发明涉及药物组合物和制备含有生长激素促分泌素作为活性成分的片剂的方法。片剂通过形成活性成分的粉末混合物制备的N- [1（R） - [（1,2-二氢-1-甲磺酰基 - 螺[3H-吲哚-3,4'- piperdin] -1'- 基）羰基] -2-（苯甲基氧基）乙基] -2-氨基-2-甲基丙酰胺，或其药学上可接受的盐，特别是甲磺酸盐，用粘合剂/稀释剂，第一稀释剂，第二稀释剂，第一部分崩解剂和润滑剂; 用乙醇/水溶液湿法制粒粉末混合物以形成颗粒; 干燥颗粒以除去乙醇/水; 加入第二部分崩解剂; 润滑颗粒; 并将干燥的颗粒压缩成所需的片剂形式。本发明还涉及该化合物的新颖的无定形形式的N- [1（R） - [（1,2-二氢-1-甲磺酰基 - 螺[3H-吲哚-3,4'- piperdin] -1'- 基）羰基] -2-（苯甲基氧基）乙基]，将其直接制作片剂制剂的处理的结果-2-氨基-2-甲基丙酰胺甲磺酸盐。

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